Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1
pubmed:dateCreated
1994-2-14
pubmed:abstractText
GYKI 52466 and related 2,3-benzodiazepines are highly selective antagonists of AMPA-evoked responses in rat CNS. However, these compounds do not compete with [3H]AMPA binding and their site of action remains unclear. Here we show that [3H]GYKI 53405 binds specifically to Xenopus brain membranes with KD and Bmax values of 4.5 microM and 35 pmol mg-1 protein respectively. Binding is increased in the presence of Mg2+ and is unaffected by AMPA or kainate. This is the first report of the binding of a GYKI 52466-related radioligand to any tissue and these results provide an initial step towards the characterization of novel recognition sites which are of considerable therapeutic potential.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Oct
pubmed:issn
0959-4965
pubmed:author
pubmed:issnType
Print
pubmed:day
25
pubmed:volume
5
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
93-4
pubmed:dateRevised
2009-9-29
pubmed:meshHeading
pubmed:year
1993
pubmed:articleTitle
Binding of the AMPA receptor antagonist [3H]GYKI 53405 to Xenopus brain membranes.
pubmed:affiliation
Department of Pharmacology, Medical School, University of Birmingham, Edgbaston, UK.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't